CETP, a hydrophobic plasma glycoprotein, is a promising target for raising circulating HDL cholesterol (HDL-C) concentrations in humans. CETP is secreted primarily from the liver and plays a critical role in HDL metabolism by facilitating the exchange of cholesteryl esters (CE) from HDL for triglycerides (TG) in apoB-containing lipoproteins, such as LDL and VLDL.

CETP catalyses the exchange of cholesteryl ester and triglyceride between HDL and apoB containing lipoprotein particles. The role of CETP in modulating plasma HDL cholesterol levels in humans is well established and there have been significant efforts to develop CETP inhibitors to increase HDL cholesterol for the treatment of coronary artery disease.